Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.

Refolding of viral class-1 membrane fusion proteins from a native state to a trimer-of-hairpins structure promotes entry of viruses into cells. Here we present the structure of the bovine leukaemia virus transmembrane glycoprotein (TM) and identify a group of asparagine residues at the membrane-dist...

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Main Authors: Daniel Lamb, Alexander W Schüttelkopf, Daan M F van Aalten, David W Brighty
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2011-02-01
Series:PLoS Pathogens
Online Access:https://journals.plos.org/plospathogens/article/file?id=10.1371/journal.ppat.1001268&type=printable
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author Daniel Lamb
Alexander W Schüttelkopf
Daan M F van Aalten
David W Brighty
author_facet Daniel Lamb
Alexander W Schüttelkopf
Daan M F van Aalten
David W Brighty
author_sort Daniel Lamb
collection DOAJ
description Refolding of viral class-1 membrane fusion proteins from a native state to a trimer-of-hairpins structure promotes entry of viruses into cells. Here we present the structure of the bovine leukaemia virus transmembrane glycoprotein (TM) and identify a group of asparagine residues at the membrane-distal end of the trimer-of-hairpins that is strikingly conserved among divergent viruses. These asparagines are not essential for surface display of pre-fusogenic envelope. Instead, substitution of these residues dramatically disrupts membrane fusion. Our data indicate that, through electrostatic interactions with a chloride ion, the asparagine residues promote assembly and profoundly stabilize the fusion-active structures that are required for viral envelope-mediated membrane fusion. Moreover, the BLV TM structure also reveals a charge-surrounded hydrophobic pocket on the central coiled coil and interactions with basic residues that cluster around this pocket are critical to membrane fusion and form a target for peptide inhibitors of envelope function. Charge-surrounded pockets and electrostatic interactions with small ions are common among class-1 fusion proteins, suggesting that small molecules that specifically target such motifs should prevent assembly of the trimer-of-hairpins and be of value as therapeutic inhibitors of viral entry.
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spelling doaj-art-899a707dd69c4f9fa149105ecc6cce1e2025-08-20T02:34:16ZengPublic Library of Science (PLoS)PLoS Pathogens1553-73661553-73742011-02-0172e100126810.1371/journal.ppat.1001268Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.Daniel LambAlexander W SchüttelkopfDaan M F van AaltenDavid W BrightyRefolding of viral class-1 membrane fusion proteins from a native state to a trimer-of-hairpins structure promotes entry of viruses into cells. Here we present the structure of the bovine leukaemia virus transmembrane glycoprotein (TM) and identify a group of asparagine residues at the membrane-distal end of the trimer-of-hairpins that is strikingly conserved among divergent viruses. These asparagines are not essential for surface display of pre-fusogenic envelope. Instead, substitution of these residues dramatically disrupts membrane fusion. Our data indicate that, through electrostatic interactions with a chloride ion, the asparagine residues promote assembly and profoundly stabilize the fusion-active structures that are required for viral envelope-mediated membrane fusion. Moreover, the BLV TM structure also reveals a charge-surrounded hydrophobic pocket on the central coiled coil and interactions with basic residues that cluster around this pocket are critical to membrane fusion and form a target for peptide inhibitors of envelope function. Charge-surrounded pockets and electrostatic interactions with small ions are common among class-1 fusion proteins, suggesting that small molecules that specifically target such motifs should prevent assembly of the trimer-of-hairpins and be of value as therapeutic inhibitors of viral entry.https://journals.plos.org/plospathogens/article/file?id=10.1371/journal.ppat.1001268&type=printable
spellingShingle Daniel Lamb
Alexander W Schüttelkopf
Daan M F van Aalten
David W Brighty
Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.
PLoS Pathogens
title Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.
title_full Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.
title_fullStr Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.
title_full_unstemmed Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.
title_short Charge-surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins.
title_sort charge surrounded pockets and electrostatic interactions with small ions modulate the activity of retroviral fusion proteins
url https://journals.plos.org/plospathogens/article/file?id=10.1371/journal.ppat.1001268&type=printable
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AT daanmfvanaalten chargesurroundedpocketsandelectrostaticinteractionswithsmallionsmodulatetheactivityofretroviralfusionproteins
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